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An asymmetric synthesis of substituted piperidines has been described.b-Cyclodextrin- or oxazaborolidine-catalyzed asymmetric reduction ofa-azido aryl ketones to the corresponding alcohols has been employed as the key step along with ring closing metathesis and selective dihydroxylation. Substituted piperidines (polyhydroxy piperidines or azasu-gars) have been identified as an important class of therapeu-tic agents in the treatment of influenza infection,1cancermetastatis,2viral infections including AIDS,3and diabetes(Fig. 1).4As a result, numerous classes of inhibitors havebeen developed, some of which provide interesting insights into the mechanism of enzymatic glycoside hydrolysis.Amongst them, both naturally occurring and syntheticpolyhydroxylated piperidines5(1–4) have been shown tobe specific and potent inhibitors of glycosidases6and have been demonstrated to have great potential as drugs for treating a variety of carbohydrate mediated diseases.7 As a consequence of this, there has been a great deal of interest, not only in the synthesis of the natural products themselves, but also that of chemically modified analogues. However, most of the methodologies have been developed for the synthesis of compounds 1and4and their stereo-isomers,8,9which can be regarded as substituted piperidines,starting from the carbohydrates and, in general, require chiral starting materials to reach the specific target. Thus the development of new methods from achiral precursors for the enantioselective synthesis of polyhydroxylated piper-idines constitutes an area of current interest.10 Herein, we wish to report the complete asymmetric synthesis of1and4starting from readily available achiral 4-methyl phenacyl bromide5. |
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NearSecond: 金币+70, ★★★★★最佳答案, 谢谢您，分给别人了一点，您没意见吧，都不容易。非常感谢。 2013-04-04 07:31:55
NearSecond: 金币+70, ★★★★★最佳答案, 谢谢您，分给别人了一点，您没意见吧，都不容易。非常感谢。 2013-04-04 07:31:55
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我们已经描述过不对称合成的取代哌啶的方法.b-环糊精或恶唑硼烷催化的不对称还原OFA-叠氮芳基酮为相应的醇已经被证明为关键步骤，伴随着闭环复分解反应和选择性双羟基化反应。 取代的哌啶（羟基哌啶或）已被确定为在在流感病毒感染、转移癌、病毒感染包括艾滋病在内和糖尿病（图1）的一类重要的治疗药物，因此，很多抑制剂都被开发了，其中一些在对酶促糖苷水解反应机制上产生很大兴趣.在这些药物当中，无论是天然存在的还是合成的多羟基哌啶都已展示出明确的作用效果是很强的糖苷酶抑制剂，并被证明有很大的潜力成为治疗多种碳水化合物介导的疾病的药物。 因此，不仅在合成的天然化合物本身，在化学修饰的类似物合成上也具有极大的兴趣。然而，大多数已被开发的方法都是用来合成被称为取代哌啶的化合物1和4and它们的立体异构体8和9，它们从碳水化合物开始并在一般情况中，需要手性起始物来达到的特定目的。因此，从非手性前体物质具有立体选择性的合成多羟基哌啶事当前我们应当发展的方向.在此，我们希望报导出从容易获得的非手性4 - 甲基苯甲酰溴化物来不对称合成化合物1和4的方法。 |
5楼2013-04-03 16:40:16
NearSecond
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2楼2013-04-02 15:54:24
3楼2013-04-02 17:13:47
NearSecond
金虫 (正式写手)
- 应助: 3 (幼儿园)
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4楼2013-04-02 17:53:25
